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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
PF-3845 (PF3845; PF 3845) is a novel, biaryl ether piperidine-based, selective and covalent/irreversible inhibitor of FAAH (fatty acid amide hydrolase) with anti-inflammatory, antidiarrheal and antinociceptive effects. It inhibits FAAH1 with a Ki of 230 nM, and showed little activity against FAAH2. Structurally, PF-3845 inhibits FAAH by forming a covalent, irreversible bond with the protein, involving carbamylating FAAH's catalytic S241 nucleophile. PF-3845 promotes neuronal survival, attenuates inflammation and improves functional recovery in mice with traumatic brain injury.
ln Vitro |
In COS-7 cells, PF-3845 (0.5 nM-10 μM; 40 min) exhibits little activity against FAAH-2 (IC50>10 μM) and inhibits human FAAH-1 (IC50=18 nM) in a concentration-dependent manner [1]. Colo-205 cell viability is considerably reduced by PF-3845 (0.1-1000 μM; 48 h)[2].
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ln Vivo |
In rats, PF-3845 (1–30 mg/kg; po) reduces inflammatory pain in a way that is dependent on cannabinoid receptors[1]. For up to 24 hours, PF-3845 (10 mg/kg; one intraperitoneal; ip) specifically inhibits FAAH in mice[1]. Anandamide (AEA) in mice is dramatically and persistently elevated with administration of PF-3845 (10 mg/kg; single ip)[1].
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Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (200g- 250g) are injected CFA[1]
Doses: 1, 3, 10, 30 mg/kg Route of Administration: Oral administration Experimental Results: Caused a dose-dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg. |
References |
[1]. Lamont Booker, et al. The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice. Br J Pharmacol, 2012, 165(8), 2485-2496.
[2]. Wasilewski A, et, al. Fatty acid amide hydrolase (FAAH) inhibitor PF-3845 reduces viability, migration and invasiveness of human colon adenocarcinoma Colo-205 cell line: an in vitro study. Acta Biochim Pol. 2017;64(3):519-525. [3]. Ahn K, et al. Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chem Biol. 2009 Apr 24;16(4):411-20. [4]. Booker L, et al. The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice. Br J Pharmacol, 2012, 165(8), 2485-2496. |
Molecular Formula |
C24H23F3N4O2
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Molecular Weight |
456.46
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CAS # |
1196109-52-0
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SMILES |
O=C(N1CCC(CC2=CC=CC(OC3=NC=C(C=C3)C(F)(F)F)=C2)CC1)NC4=CN=CC=C4
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1908 mL | 10.9539 mL | 21.9077 mL | |
5 mM | 0.4382 mL | 2.1908 mL | 4.3815 mL | |
10 mM | 0.2191 mL | 1.0954 mL | 2.1908 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.